Article

Influence of ginsenoside Rh1 and F1 on human cytochrome p450 enzymes.

Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, The Chinese Academy of Sciences, 457 Zhong-shan Road, Dalian 116023, P. R. China.
Planta Medica (impact factor: 2.15). 03/2006; 72(2):126-31. DOI:10.1055/s-2005-873197 pp.126-31
Source: PubMed

ABSTRACT For an oral herbal medicine, the components that can enter the systemic circulation may be the really effective components. In the present study, the effects on the human cytochrome P450 activities of ginsenoside Rb (1) and two hydrolysis products of 20( S)-protopanaxatriol ginsenosides in humans, namely ginsenoside Rh (1) and F (1), which may reach the systemic circulation after oral administration of ginseng extract, were evaluated. Our results showed that Rb (1) exhibited no marked effects on the activities of human cytochrome P450, whereas Rh (1) and F (1) exhibited competitive inhibition of the activity of CYP3A4 with K(i) values of 57.7 +/- 9.6 microM and 67.8 +/- 16.2 microM, respectively. F (1) also exhibited a weaker inhibition of the activity of CYP2D6. Rh (1) exhibited a weak stimulation rather than an inhibition of the activity of CYP2E1. The degradation of ginsenosides in the gastrointestinal tract may play an important role in the ginseng-associated drug-drug interactions, but the effects might be not due to Rh (1) and F (1).

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Keywords

20( S)-protopanaxatriol ginsenosides
 
gastrointestinal tract
 
ginseng
 
ginseng-associated drug-drug interactions
 
ginsenoside Rb
 
ginsenoside Rh
 
ginsenosides
 
human cytochrome P450
 
human cytochrome P450 activities
 
hydrolysis products
 
marked effects
 
oral administration
 
oral herbal medicine
 
Rh
 
systemic circulation
 
weaker inhibition